Phenibut (beta-phenyl-gamma-aminobutyric acid) is a neuropsychotropic discovered through Soviet research and introduced into general clinical practice in Russia in the 1960’s. Not unlike picamilon, it was initially designed with Soviet cosmonauts in mind. As such, it needed to be anxiolytic (anxiety relieving) while at the same time acting as a focusing agent.
The story of Phenibut’s development begins in 1963, in St.Petersburg, Russia. A Soviet Union lab scientist by the name of Perekalin synthesized 3-phenyl-4-aminobutyric acid, an experimental drug intended to calm children with certain psychiatric conditions. Professor Khaunma, one of the scientists working on the project, named the drug Phenigamma and wrote about the tranquilizing properties of phenibut in the Byulleten Eksperimental’noi Biologii i Meditsiny.
By 1975, Phenigamma’s use had spread from clinical trials and practice to use by the public, as well as being mandated for use by cosmonauts in the Soviet Ministry. By the turn of the 21st century, over 300 papers had been written about Phenibut’s properties and over the past several years it has grown in popularity worldwide. It is often sold alongside nootropics and other health supplements by various online vendors in generic powder and branded pill forms.
The secret to Phenibut’s potency (beta-phenyl-gamma-aminobutyric acid) lies in its unique molecular structure involving GABA and an attached phenyl ring. GABA (gamma-aminobutyric acid) is the brain’s primary inhibitory neurotransmitter however it cannot easily cross the blood-brain-barrier. Phenibut, due to the addition of a phenyl group, can easily pass through the blood-brain-barrier and bind to the GABA receptors. As a result, Phenibut effectively delivers GABAergic activity to the brain causing psychotropic inhibitory actions.
Phenibut has a half-life of around 5 hours but it is important to note that some people metabolize the substance differently so this may vary amongst users. Some users also report that the full effects aren’t felt until three to four hours after dosing. It’s important to wait at least four hours to gauge effects before you try to re-dose this substance. Some people report being drowsy up to 24 hours after their last dose and this risk increases as the dosage is increased. Phenibut can cause tolerance to build up quickly and habituation can lead to a situation of “free floating anxiety” so cycling it and using sparingly is recommended to avoid tolerance and addiction.
Phenibut is not only an analogue of GABA, but also an analogue of the muscle relaxant drug baclofen (β-(4-chlorophenyl)-GABA), as well as pregabalin (β-isobutyl-GABA), and GABOB (β-hydroxy-GABA). Phenibut is a GABA-b receptor agonist which targets the same inhibitory receptors as alcohol and various other substances such as listed above. It is interesting to note that the famous nootropic, piracetam is also a derivative of GABA (cyclic) however it does not share the same pharmacology or effects as Phenibut or any GABAergic for that matter.
So Why is Phenibut Labelled as a Nootropic?
There is some controversy as to whether or not Phenibut is actually a nootropic substance. In multiple journal articles, it’s referred to as a nootropic substance. Technically, it does not fit the criteria due to its psychotropic and potentially addictive nature. Although it is a sedative agent, some may argue that Phenibut works as a nootropic at lower dosages by lowering stress and anxiety thresholds since these factors may interfere with cognitive performance.
Cetyl GABA, lithium hydroxybutyrates and Phenibut were all shown in rodent trials to decrease retrograde amnesia that resulted from electric shock in passive avoidance performance tests. Phenibut and the others performed about as well as piracetam itself. The important factor seems to be dosing here, doses that induce CNS depression and muscle relaxation seem to overshoot the therapeutic nootropic benefit. Phenibut is still a popular treatment used in Russia to treat stress, reduce anxiety, improve sleep and even to treat PTSD.
Phenibut acts as a GABA-b agonist, which means it activates certain GABA receptors which is the source of it’s anxiolytic effect. Unlike many other GABA substances, Phenibut also has a dopaminergic effect by stimulating certain dopamine receptors. This may add to Phenibut’s nootropic effects as well as to its addictive qualities. It also antagonizes beta-PEA (phenethylamine), an endogenous anxiogenic (causing anxiety) compound.
As a GABA-B receptor agonist Phenibut operates via inhibitory action by reducing post-synaptic neuronal firing rate. It’s this post-synaptic inhibition that results in the anxiety relief, sedation and/or muscle relaxation from Phenibut. By 2001 there were over 300 scientific publications featuring studies on Phenibut’s nootropic and pharmacological properties. Unfortunately most of these are in untranslated Russian, which may prove problematic for researchers not fluent in that language. Phenibut is known to have a plasma half-life of just over 5 hours, but the lingering after effects can last throughout the day at higher doses.
Phenibut is also anti-hypoxic. When you train a muscle intensely and it can’t get enough oxygen anymore it can become hypoxic. This metabolic stress can lead to muscle hypertrophy. As a result, Phenibut has been used by body builders to increase tolerance to metabolic stress.
Phenibut should not be considered a typical nootropic or performance enhancer and it’s habituation danger should not be underestimated. Also, it should be noted that in the majority of human studies, doses never exceeded 3 grams a day. It is prudent to only take the minimum effective dose if you’re attempting to use Phenibut for focus or stress relief.
Use of Phenibut daily and/or in doses of a few grams a day several days a week have been shown to lead to bad results as is witnessed anecdotally throughout the internet and in the scientific literature. In many cases, using ranges higher than 3 grams a day without cycling, are anecdotally responsible for severe withdrawal symptoms akin to that of alcoholism or benzodiazepine habituation. In the medical literature there are however extreme cases of addiction and abuse that have led to side effects as severe as tremors, seizures, free-floating anxiety, insomnia or psychosis so use sparingly at the minimum effective dose.
It is important to note that nootropics have not been approved by the FDA and that there are still dangers to consuming these substances. Although many have been shown in studies to be generally safe, consuming is not without risk. Adverse side effects and allergic reactions are possible so that must be taken into account. Every nootropic should be reviewed and allowed by a doctor as there is always some level of risk.
Nootropics are not approved to treat or manage any medical condition. Always check with your personal care provider before attempting any exercise, workout or supplement regimen especially if you are currently under a doctor’s care or taking any over-the-counter or prescribed medicines.
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